AR7

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Chemical Structure| 80306-38-3 同义名 : -
CAS号 : 80306-38-3
货号 : A857996
分子式 : C15H12ClNO
纯度 : 99%+
分子量 : 257.715
MDL号 : MFCD27978377
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(97.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Retinoic acid (RA), the major bioactive metabolite of retinol or vitamin A, induces a spectrum of pleiotropic effects in cell growth and differentiation that are related to embryonic development and adult physiology. The RA activity is mediated primarily by members of the retinoic acid receptor (RAR) subfamily, namely RARα, RARβ and RARγ, which belong to the nuclear receptor (NR) superfamily of transcription factors[1]. Atypical retinoid 7 (AR7) is a retinoic acid receptor α (RARα) antagonist and also acts as chaperone-mediated autophagy (CMA) activator. AR7 dose-dependently activates CMA activity in mouse fibroblasts expressing the KFERQ-mcherry1 photoactivable reporter. In Parkinson disease, mutant LRRK2 perturbs chaperone-mediated-autophagy (CMA) to degrade α-synuclein. AR7 treatment in 24 h dose-dependently, induced neuronal LAMP2A transcription and lysosomal activity in mouse embryonic fibroblasts (MEFs). AR7 at 20 μM also attenuated the progressive accumulation of both intracellular and extracellular α-synuclein oligomers in prolonged cultures of mutant cortical neurons (DIV21), indicating that oligomer accumulation can be suppressed by CMA activation[2].
作用机制 AR-7 is docked to a hydrophobic region of the RARα-binding pocket formed by h3, h10 and h12[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.88mL

0.78mL

0.39mL

19.40mL

3.88mL

1.94mL

38.80mL

7.76mL

3.88mL
参考文献

[1]di Masi A, Leboffe L, De Marinis E, et al. Retinoic acid receptors: from molecular mechanisms to cancer therapy. Mol Aspects Med. 2015;41:1‐115.

[2]Ho PW, Leung CT, Liu H, et al. Age-dependent accumulation of oligomeric SNCA/α-synuclein from impaired degradation in mutant LRRK2 knockin mouse model of Parkinson disease: role for therapeutic activation of chaperone-mediated autophagy (CMA). Autophagy. 2020;16(2):347‐370.

[3]Anguiano J, Garner TP, Mahalingam M, Das BC, Gavathiotis E, Cuervo AM. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives [published correction appears in Nat Chem Biol. 2013 Nov;9(11):746]. Nat Chem Biol. 2013;9(6):374‐382.